Synthesis and anticonvulsant activity of some newer dihydro-pyrimidine-5-carbonitrile derivatives: Part II

ObjectivesTo synthesize dihydro-pyrimidine-5-carbonitrile derivatives (5–23), as an extension of the previous series, and to evaluate their anticonvulsant potential.MethodsThe designed compounds were synthesized and characterized using infrared (IR), nuclear magnetic resonance (NMR) and mass spectroscopy and were evaluated for anticonvulsant activity using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) methods. Compounds with appreciable activity were investigated for their neurotoxicity using the rotarod test.ResultsCompounds 17 and 23 were found to be most active at a dose of 30 mg kg−1 at 0.5 h and 4 h in both models and did not exhibit motor impairment activity, even at higher doses.ConclusionThe newer designed compounds were found to be better than previously reported compounds. This study also shows that increased lipophilicity is directly related to the anticonvulsant activity.